Drug-induced QT interval prolongation - Regulatory guidance and perspectives on hERG channel studies

Novartis Foundation Symposium

Volumn 266, Issue , 2005, Pages 251-280

  Shah, Rashmi R ^a  

^a MEDICINES AND HEALTHCARE PRODUCTS REGULATORY AGENCY   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIARRHYTHMIC AGENT; VOLTAGE GATED POTASSIUM CHANNEL;

ACTION POTENTIAL; CHEMICALLY INDUCED DISORDER; DRUG EFFECT; DRUG LEGISLATION; HEART ARRHYTHMIA; HUMAN; LONG QT SYNDROME; MANAGEMENT; PATHOLOGY; PHYSIOLOGY; REVIEW; RISK ASSESSMENT; TORSADE DES POINTES;

ACTION POTENTIALS; ANTI-ARRHYTHMIA AGENTS; ARRHYTHMIA; HUMANS; LEGISLATION, DRUG; LONG QT SYNDROME; POLICY MAKING; POTASSIUM CHANNELS, VOLTAGE-GATED; RISK ASSESSMENT; TORSADES DE POINTES;

EID: 23844542866     PISSN: 15282511     EISSN: None     Source Type: Book Series    
DOI: None     Document Type: Conference Paper

References (106)

1. Abbott GW, Goldstein SA 2002 Disease-associated mutations in KCNE potassium channel subunits (MiRPs) reveal promiscuous disruption of multiple currents and conservation of mechanism. FASEB J 16:390-400
2. Kr potassium channels with HERG and is associated with cardiac arrhythmias. Cell 97:175-187
3. Abbott GW, Goldstein SAN, Sesti F 2001 Do all voltage-gated potassium channels use miRPs? Circ Res 88:981-983
4. Anantharam A, Lewis A, Panaghie G et al 2003a RNA interference reveals that endogenous Xenopus minK-related peptides govern mammalian K+ channel function in oocytes expression studies. J Biol Chem 278:11739-11745
5. Anantharam A, Markowitz SM, Abbott GW 2003b Pharmacogenetic considerations in diseases of cardiac ion channels. J Pharmacol Exp Ther 307:831-838
6. Arnt J 1998 Pharmacological differentiation of classical and novel antipsychotics. Int Clin Psychopharmacol 13(suppl 3):S7-14
7. Bartsch W, Sponer G, Strein K et al 1990 Pharmacological characteristics of the stereoisomers of carvedilol. Eur J Clin Pharmacol 38(suppl 2):S104-107
8. Bayer R, Schwarzmaler J, Pernice R 1988 Basic mechanism underlying prenylamine-induced torsade de pointes: differences between prenylamine and fendiline due to basic actions of the isomers. Curr Med Res Opin 11:254-272
9. Ben-David J, Zipes DP 1990 α-Adrenoceptor stimulation and blockade modulates cesium-induced early afterdepolarizations and ventricular tachyarrhythmias in dogs. Circulation 82:225-233
10. Bezzina CR, Verkerk AO, Busjahn A et al 2003 A common polymorphism in KCNH2 (HERG) hastens cardiac repolarization. Cardiovasc Res 59:27-36
11. Carlsson L, Amos GJ, Andersson B, Drews L, Duker G, Wadstedt G 1997 Electrophysiological characterization of the prokinetic agents cisapride and mosapride in vivo and in vitro: implications for proarrhythmic potential? J Pharmacol Exp Ther 282:220-227
12. Cavero I, Crumb W 2001 Native and cloned ion channels from human heart: laboratory models for evaluating the cardiac safety of new drugs. Eur Heart J Suppl 3(suppl K):K53-K63
13. Chachin M, Kurachi Y 2002 Evaluation of pro-arrhythmic risk of drugs due to QT interval prolongation by the HERG expression system [Japanese]. Nippon Yakurigaku Zasshi 119:345-351
14. Chen J, Seebohm G, Sanguinetti MC 2002 Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels. Proc Natl Acad Sci USA 99:12461-12466
15. Danielsson BR, Lansdell K, Patmore L, Tomson T 2003 Phenytoin and phenobarbital inhibit human HERG potassium channels. Epilepsy Res 55:147-157
16. Delgado LF, Pferferman A, Sole D, Naspitz CK 1998 Evaluation of the potential cardiotoxicity of the antihistamines terfenadine, astemizole, loratadine, and cetirizine in atopic children. Ann Allergy Asthma Immunol 80:333-337
17. Dong DL, Li Z, Wang HJ, Du ZM, Song WH, Yang BF 2004 Acidification alters antiarrhythmic drug blockade of the ether-a-go-go gene (HERG) channels. Pharmacol Toxicol 94:209-212
18. Drolet B, Vincent F, Rail J et al 1999 Thioridazine lengthens repolarization of cardiac ventricular myocytes by blocking the delayed rectifier potassium current. J Pharmacol Exp Ther 288:1261-1268
19. Drolet B, Simard C, Roden DM 2004 Unusual effects of a QT-prolonging drug, arsenic trioxide, on cardiac potassium currents. Circulation 109:26-29
20. Eckardt L, Breithardt G, Haverkamp W 2002 Electrophysiologic characterization of the antipsychotic drug sertindole in a rabbit heart model of torsade de pointes: low torsadogenic potential despite QT prolongation. J Pharmacol Exp Ther 300:64-71
21. Ehrlich JR, Pourrier M, Weerapura M et al 2004 KvLQT1 modulates the distribution and biophysical properties of HERG: a novel alpha-subunit interaction between delayed-rectifier currents. J Biol Chem 279:1233-1241
22. Endo J, Nomura M, Morishita S et al 2002 Influence of mosapride citrate on gastric motility and autonomic nervous function: evaluation by spectral analyses of heart rate and blood pressure variabilities, and by electrogastrography. J Gastroenterol 37:888-895
23. Ficker E, Thomas D, Viswanathan PC et al 2000 Novel characteristics of a misprocessed mutant HERG channel linked to hereditary long QT syndrome. Am J Physiol Heart Circ Physiol 279:H1748-H1756
24. Ficker E, Dennis AT, Wang L, Brown AM 2003 Role of the cytosolic chaperones Hsp70 and Hsp90 in maturation of the cardiac potassium channel HERG. Circ Res 92:87-100
25. Ficker E, Kuryshev YA, Dennis AT et al 2004 Mechanisms of arsenic-induced prolongation of cardiac repolarization. Mol Pharmacol 66:33-44
26. 3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur J Pharmacol 430:147-148
27. Fossa AA, Wisialowski T, Wolfgang E et al 2004 Differential effect of HERG blocking agents on cardiac electrical alternans in the guinea pig. Eur J Pharmacol 486:209-221
28. Friederich P, Solth A, Schillemeit S, Isbrandt D 2004 Local anaesthetic sensitivities of cloned HERG channels from human heart: comparison with HERG/MiRP1 and HERG/MiRP1 T8A. Br J Anaesth 92:93-101
29. Furushima H, Chinushi M, Washizuka T, Aizawa Y 2001 Role of α1-blockade in congenital long QT syndrome - investigation by exercise stress test. Jpn Circ J 65:654-658
30. Furutani M, Trudeau MC, Hagiwara N et al 1999 Novel mechanism associated with an inherited cardiac arrhythmia: defective protein trafficking by the mutant HERG (G601S) potassium channel. Circulation 99:2290-2294
31. Fung MC, Hsiao-hui Wu H, Kwong K, Hornbuckle K, Muniz E 2000 Evaluation of the profile of patients with QTc prolongation in spontaneous adverse event reporting over the past three decades - 1969-1998. Pharmacoepidemiol Drug Safety 9(suppl 1):S24-25
32. Gilbert JD, Cahill SA, McCartney DG, Lukas A, Gross GJ 2000 Predictors of torsades de pointes in rabbit ventricles perfused with sedating and nonsedating histamine H1-receptor antagonists. Can J Physiol Pharmacol 78:407-414
33. Gonzalez T, Arias C, Caballero R et al 2002 Effects of levobupivacaine, ropivacaine and bupivacaine on HERG channels: stereoselective bupivacaine block. Br J Pharmacol 137:1269-1279
34. Graf BM, Abraham I, Eberbach N, Kunst G, Stowe DF, Martin E 2002 Differences in cardiotoxicity of bupivacaine and ropivacaine are the result of physicochemical and stereoselective properties. Anesthesiology 96:1427-1434
35. Gristwood RW 2002 Cardiac and CNS toxicity of levobupivacaine: strengths of evidence for advantage over bupivacaine. Drug Saf 25:153-163
36. Hagiwara T, Satoh S, Kasai Y, Takasuna K 2001 A comparative study of the fluoroquinolone antibacterial agents on the action potential duration in guinea pig ventricular myocardia. Jpn J Pharmacol 87:231-234
37. Hartigan-Go K, Bateman DN, Nyberg G, Martensson E, Thomas SH 1996a Concentration-related pharmacodynamic effects of thioridazine and its metabolites in humans. Clin Pharmacol Ther 60:543-553
38. Hartigan-Go K, Bateman ND, Daly AK, Thomas SHL 1996b Stereoselective cardiotoxic effects of terodiline. Clin Pharmacol Ther 60:89-98
39. Hondeghem LM, Hoffmann P 2003 Blinded test in isolated female rabbit heart reliably identifies action potential duration prolongation and proarrhythmic drugs: importance of triangulation, reverse use dependence, and instability. J Cardiovasc Pharmacol 41:14-24
40. Isbrandt D, Friederich P, Solth A et al 2002 Identification and functional characterization of a novel KCNE2 (MiRP1) mutation that alters HERG channel kinetics. J Mol Med 80:524-532
41. Kr. Circulation 94:2938-2946
42. + channel HERG. Mol Pharmacol 59:122-126
43. + channels. Eur J Pharmacol 458:25-29
44. Kang J, Chen XL, Wang H et al 2004 Cardiac ion channel effects of tolterodine. J Pharmacol Exp Ther 308:935-940
45. Karle CA, Kreye VA, Thomas D et al 2001 Antiarrhythmic drug carvedilol inhibits HERG potassium channels. Cardiovasc Res 49:361-370
46. + currents. J Pharmacol Exp Ther 303:688-694
47. Katoh T, Saitoh H, Ohno N et al 2003 Drug interaction between mosapride and erythromycin without electrocardiographic changes. Jpn Heart J 44:225-234
48. Keating MT, Sanguinetti MC 2001 Molecular and cellular mechanisms of cardiac arrhythmias. Cell 104:569-580
49. Kerr GD, Ingham G 1990 Torsade de pointes associated with perhexiline maleate therapy. Aust N Z J Med 20:818-820
50. Kii Y, Ito T 1997 Effects of 5-HT4-receptor agonists, cisapride, mosapride citrate, and zacopride, on cardiac action potentials in guinea pig isolated papillary muscles. J Cardiovasc Pharmacol 29:670-675
51. Kongsamut S, Kang J, Chen XL, Roehr J, Rampe D 2002 A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. Eur J Pharmacol 450:37-41
52. Kr drug response is modulated by KCR1 in transfected cardiac and noncardiac cell lines. FASEB J 17:2263-2265
53. Kuryshev YA, Ficker E, Wang L et al 2005 Pentamidine-induced long QT syndrome and block of hERG trafficking. J Pharmacol Exp Ther 312:316-323
54. Leishman DJ, Helliwell R, Wakerell J, Wallis RM 2001 Effect of E-4031, cisapride, terfenadine and terodiline on cardiac repolarization in canine Purkinje fibre and HERG channels expressed in HEK293 cells. Br J Pharmacol 133:130P
55. Llerena A, Berecz R, de la Rubia A, Dorado P 2002 QTc interval lengthening is related to CYP2D6 hydroxylation capacity and plasma concentration of thioridazine in patients. J Psychopharmacol 16:361-364
56. Lu HR, Remeysen P, De Clerck F 2000 Nonselective IKr-blockers do not induce torsades de pointes in the anesthetized rabbit during alpha1-adrenoceptor stimulation. J Cardiovasc Pharmacol 36:728-736
57. Maginn M, Frederiksen K, Adamantidis MM, Bischoff U, Matz J 2000 The effects of sertindole and its metabolites on cardiac ion channels and action potentials. J Physiol 525: 79P
58. Martin RL, McDermott JS, Salmen HJ, Palmatier J, Cox BF, Gintant GA 2004 The utility of hERG and repolarization assays in evaluating delayed cardiac repolarization: influence of multi-channel block. J Cardiovasc Pharmacol 43:369-379
59. Mbai M, Rajamani S, January CT 2002 The anti-malarial drug halofantrine and its metabolite N-desbutylhalofantrine block HERG potassium channels. Cardiovasc Res 55:799-805
60. Milon D, Daubert JC, Saint-Marc C, Gouffault J 1982 Torsade de pointes. Apropos of 54 cases [French]. Ann Fr Anesth Reanim 1:513-520
61. Mitcheson JS, Chen J, Lin M, Culberson C, Sanguinetti MC 2000 A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci USA 97:12329-12333
62. Moore N, Hall G, Sturkenboom M, Mann R, Lagnaoui R, Begaud B 2003 Biases affecting the proportional reporting ratio (PRR) in spontaneous reports pharmacovigilance databases: the example of sertindole. Pharmacoepidemiol Drug Safety 12:271-281
63. Nakaya H 2003 Electropharmacological assessment of the risk of drug-induced long-QT syndrome using native cardiac cells and cultured cells expressing HERG channels [Japanese]. Nippon Yakurigaku Zasshi 121:384-392
64. Netzer R, Bischoff U, Ebneth A 2003 HTS techniques to investigate the potential effects of compounds on cardiac ion channels at early-stages of drug discovery. Curr Opin Drug Discovery Dev 6:462-469
65. Noda T, Takaki H, Kurita T et al 2002 Gene-specific response of dynamic ventricular repolarization to sympathetic stimulation in LQT1, LQT2 and LQT3 forms of congenital long QT syndrome. Eur Heart J 23:975-983
66. Ohki R, Takahashi M, Mizuno O et al 2001 Torsades de pointes ventricular tachycardia induced by mosapride and flecainide in the presence of hypokalemia. Pacing Clin Electrophysiol 24:119-121
67. Paulussen AD, Gilissen RA, Armstrong M et al 2004 Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients. J Mol Med 82:182-188
68. + currents in mammalian cell lines and cardiac myocytes. Pflügers Arch 437:381-392
69. Pietila E, Fodstad H, Niskasaari Eet al 2002 Association between HERG K897T polymorphism and QT interval prolongation in middle-aged Finnish women. J Am Coll Cardiol 40:511-514
70. + channel. J Pharmacol Exp Ther 299:1007-1012
71. Rampe D, Murawsky MK, Grau J, Lewis EW 1998 The antipsychotic agent sertindole is a high affinity antagonist of the human cardiac potassium channel HERG. J Pharmacol Exp Ther 286:788-793
72. Redfern WS, Carlsson L, Davis AS et al 2003 Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development. Cardiovasc Res 58:32-45
73. Roden DM 2004 Drug-induced prolongation of the QT interval. N Engl J Med 350:1013-1022
74. Roy M, Dumaine R, Brown AM 1996 HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine. Circulation 94:817-823
75. Salle P, Rey JL, Bernasconi P, Quiret JC, Lombaert M 1985 Torsades de pointe. Apropos of 60 cases [French]. Ann Cardiol Angeiol (Paris) 34:381-388
76. Kr potassium channel. Cell 81:299-307
77. Scherer CR, Lerche C, Decher N et al 2002 The antihistamine fexofenadine does not affect IKr currents in a case report of drug-induced cardiac arrhythmia. Br J Pharmacol 137:892-900
78. Schroeder BC, Waldegger S, Fehr S et al 2000 A constitutively open potassium channel formed by KCNQ1 and KCNE3. Nature 403:196-199
79. Sesti F, Abbott GW, Wei J et al 2000 A common polymorphism associated with antibiotic-induced cardiac arrhythmia. Proc Natl Acad Sci USA 97:10613-10618
80. Shah RR 2002a The significance of QT interval in drug development. Br J Clin Pharmacol 54:188-202
81. Shah RR 2002b Drug-induced prolongation of the QT interval: regulatory dilemmas and implications for approval and labelling of a new chemical entity. Fundam Clin Pharmacol 16:147-156
82. Shah RR 2004 Pharmacogenetic aspects of drug-Induced torsade de pointes: potential tool for improving clinical drug development and prescribing. Drug Saf 27:145-172
83. Simons FE, Silas P, Portnoy JM, Catuogno J, Chapman D, OlufadeAO2003 Safety of cetirizine in infants 6 to 11 months of age: a randomized, double-blind, placebo-controlled study. J Allergy Clin Immunol 111:1244-1248
84. Splawski I, Shen J, Timothy KW et al 2000 Spectrum of mutations in long QT syndrome genes KVLQT1, HERG, SCN5A, KCNE1 and KCNE2. Circulation 102:1178-1185
85. + channels as pharmacological targets: present and future implications. Biochem Pharmacol 55:1741-1746
86. + channel block-related cardiotoxicity by the H1 receptor blocker cetirizine compared with other second-generation antihistamines. Mol Pharmacol 54:113-121
87. Teng S, Ma L, Zhen Y et al 2003 Novel gene hKCNE4 slows the activation of the KCNQ1 chain. Biochem Biophys Res Commun 303:808-813
88. Thanaccody R, Daly AK, Thomas SH 2003 Influence of CYP2D6 genotype on the QTc interval and plasma concentrations of thioridazine and its metabolites in psychiatric patients taking chronic therapy. Clin Pharmacol Ther 73:77
89. Thomas D, Gut B, Wendt-Nordahl G, Kiehn J 2002 The antidepressant drug fluoxetine is an inhibitor of human ether-a-go-go-related gene (HERG) potassium channels. J Pharmacol Exp Ther 300:543-548
90. Thomas D, Kiehn J, Katus HA, Karle CA 2003 Defective protein trafficking in hERG-associated hereditary long QT syndrome (LQT2): molecular mechanisms and restoration of intracellular protein processing. Cardiovasc Res 60:235-241
91. Thomas D, Wimmer AB, Wu K et al 2004 Inhibition of human ether-a-go-go-related gene potassium channels by alpha1-adrenoceptor antagonists prazosin, doxazosin and terazosin. Naunyn Schmiedebergs Arch Pharmacol 369:462-472
92. Tinel N, Diochot S, Borsotto M, Lazdunski M, Barhanin J 2000 KCNE2 confers background current characteristics to the cardiac KCNQ1 potassium channel. EMBO J 19:6326-6330
93. Toumi M, Auquier P, Francois C 2002 The safety and tolerability of sertindole in a patient name use program. Pharmacoepidemiol Drug Safety 11(suppl 1):S115
94. Tseng GN 2001 IKr: the hERG channel. J Mol Cell Cardiol 33:835-849
95. Urao N, Shiraishi H, Ishibashi K et al 2004 Idiopathic long QT syndrome with early after depolarizations induced by epinephrine. Circ J 68:587-591
96. Volperian VR, Zhou Z, Mohammad S, Hoon TJ, Studenik C, January CT 1996 Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole. J Am Coll Cardiol 28:1556-1561
97. Walker BD, Valenzuela SM, Singleton CB et al 1999 Inhibition of HERG channels stably expressed in a mammalian cell line by the antianginal agent perhexiline maleate. Br J Pharmacol 127:243-251
98. Webster R, Leishman D, Walker D 2002 Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Current Opinion Drug Disc Dev 5:116-126
99. Weerapura M, Nattel S, Chartier D, Caballero R, Hebert TE 2002 A comparison of currents carried by HERG, with and without coexpression of MiRP1, and the native rapid delayed rectifier current. Is MiRP1 the missing link? J Physiol 540:15-27
100. + channels expressed in mammalian cell lines and Xenopus oocytes. J Pharmacol Toxicol Methods 48:65-80
101. Witchel HJ, Pabbathi VK, Hofmann G, Paul AA, Hancox JC 2002b Inhibitory actions of the selective serotonin re-uptake inhibitor citalopram on HERG and ventricular L-type calcium currents. FEBS Lett 512:59-66
102. Wyte CD, Berk WA 1991 Severe oral phenytoin overdose does not cause cardiovascular morbidity. Ann Emerg Med 20:508-512
103. Yang T, Snyders D, Roden DM 2001 Drug block of IKr: model systems and relevance to human arrhythmias. J Cardiovasc Pharmacol 38:737-744
104. Yap YG, Camm AJ 2002 Potential cardiac toxicity of H1-antihistamines. Clin Allergy Immunol 17:389-419
105. Zhou Z, Volperian VR, Gong Q, Zhang S, January CT 1999 Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol 10:836-843
106. Zhou J, Meng R, Li X, Lu C, Fan S, Yang B 2003 The effect of arsenic trioxide on QT interval prolongation during APL therapy. Chin Med J (Engl) 116:1764-1766